CA3102214A1 - Ligands to cereblon (crbn) - Google Patents
Ligands to cereblon (crbn) Download PDFInfo
- Publication number
- CA3102214A1 CA3102214A1 CA3102214A CA3102214A CA3102214A1 CA 3102214 A1 CA3102214 A1 CA 3102214A1 CA 3102214 A CA3102214 A CA 3102214A CA 3102214 A CA3102214 A CA 3102214A CA 3102214 A1 CA3102214 A1 CA 3102214A1
- Authority
- CA
- Canada
- Prior art keywords
- compound
- optionally substituted
- formula
- mmol
- pharmaceutically acceptable
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Immunology (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862692167P | 2018-06-29 | 2018-06-29 | |
| US62/692,167 | 2018-06-29 | ||
| PCT/US2019/039555 WO2020006264A1 (en) | 2018-06-29 | 2019-06-27 | Ligands to cereblon (crbn) |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3102214A1 true CA3102214A1 (en) | 2020-01-02 |
Family
ID=68987146
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3102214A Pending CA3102214A1 (en) | 2018-06-29 | 2019-06-27 | Ligands to cereblon (crbn) |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US11530219B2 (enExample) |
| EP (1) | EP3813829A4 (enExample) |
| JP (2) | JP7321194B2 (enExample) |
| KR (2) | KR20210025061A (enExample) |
| CN (1) | CN112638380B (enExample) |
| AU (1) | AU2019294835B2 (enExample) |
| CA (1) | CA3102214A1 (enExample) |
| WO (1) | WO2020006264A1 (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20190136125A (ko) | 2012-12-21 | 2019-12-09 | 국립연구개발법인 양자과학기술연구개발기구 | 뇌 안에 축적된 타우 단백질을 이미징하기 위한 신규한 화합물 |
| CN111372585A (zh) | 2017-11-16 | 2020-07-03 | C4医药公司 | 用于靶蛋白降解的降解剂和降解决定子 |
| KR20210018199A (ko) | 2018-03-26 | 2021-02-17 | 씨4 테라퓨틱스, 인코포레이티드 | 이카로스의 분해를 위한 세레블론 결합제 |
| WO2019204354A1 (en) | 2018-04-16 | 2019-10-24 | C4 Therapeutics, Inc. | Spirocyclic compounds |
| JP7293343B2 (ja) | 2018-05-09 | 2023-06-19 | アプリノイア セラピューティクス リミテッド | ヘテロアリール化合物及びその使用 |
| WO2020006264A1 (en) * | 2018-06-29 | 2020-01-02 | Dana-Farber Cancer Institute, Inc. | Ligands to cereblon (crbn) |
| US12582641B2 (en) | 2019-02-25 | 2026-03-24 | Shanghaitech University | Sulfur-containing compound based on glutarimide skeleton and application thereof |
| CN112321566B (zh) | 2019-08-05 | 2022-06-10 | 上海科技大学 | Egfr蛋白降解剂及其抗肿瘤应用 |
| CA3161455A1 (en) | 2019-11-13 | 2021-05-20 | Aprinoia Therapeutics Limited | Compounds for degrading tau protein aggregates and uses thereof |
| US20230111853A1 (en) * | 2019-12-17 | 2023-04-13 | Orionis Biosciences, Inc. | Compounds modulating protein recruitment and/or degradation |
| ES2980575T3 (es) | 2019-12-18 | 2024-10-02 | Novartis Ag | Derivados de 3-(5-metoxi-1-oxoisoindolin-2-il)piperidin-2,6-diona y usos de los mismos |
| CN113582980B (zh) * | 2020-04-30 | 2023-11-24 | 上海科技大学 | 基于杂环和戊二酰亚胺骨架的化合物及其应用 |
| JP2024504932A (ja) | 2021-01-13 | 2024-02-02 | モンテ ローザ セラピューティクス， インコーポレイテッド | イソインドリノン化合物 |
| AU2022271290A1 (en) | 2021-05-07 | 2023-11-23 | Kymera Therapeutics, Inc. | Cdk2 degraders and uses thereof |
| CR20230614A (es) | 2021-06-03 | 2024-02-01 | Novartis Ag | Derivados de 3-(1-oxoisoindolin-2-il)piperidina-2,6-diona y sus usos médicos |
| CN115504963A (zh) * | 2021-06-22 | 2022-12-23 | 苏州开拓药业股份有限公司 | 一种c-Myc蛋白降解剂 |
| WO2022272061A1 (en) * | 2021-06-25 | 2022-12-29 | Celgene Corporation | Cereblon binding compounds, compositions thereof, and methods of treatment therewith |
| US20250066325A1 (en) * | 2021-11-04 | 2025-02-27 | The Brigham And Women's Hospital, Inc. | Directed degron molecules and applications thereof |
| AU2022419982B2 (en) * | 2021-12-22 | 2026-04-16 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| CA3237577A1 (en) * | 2021-12-22 | 2023-06-29 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| KR102738668B1 (ko) | 2022-02-25 | 2024-12-06 | 계명대학교 산학협력단 | 항암 활성을 갖는 신규 화합물 및 이의 용도 |
| EP4493554A1 (en) | 2022-03-17 | 2025-01-22 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| CA3249074A1 (en) | 2022-06-06 | 2023-12-14 | C4 Therapeutics, Inc. | BICYCLIC SUBSTITUTION GLUTARIMIDE CEREBLON BINDERS |
| WO2024032689A1 (zh) * | 2022-08-10 | 2024-02-15 | 标新生物医药科技(上海)有限公司 | 基于异吲哚啉取代戊二酰亚胺骨架的化合物及其应用 |
| PE20251697A1 (es) | 2022-11-04 | 2025-07-02 | Bristol Myers Squibb Co | Compuestos y su uso para el tratamiento de hemoglobinopatias |
| WO2024167423A1 (en) * | 2023-02-07 | 2024-08-15 | Captor Therapeutics S.A. | Gspt1 degrader compounds |
| WO2024238872A2 (en) * | 2023-05-18 | 2024-11-21 | Firefly Bio, Inc. | Isoindolinone-glutarimide antibody conjugates, and uses thereof |
| WO2025101912A1 (en) * | 2023-11-09 | 2025-05-15 | The Board Of Trustees Of The Leland Stanford Junior University | Hells helicase degraders and uses thereof |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030045552A1 (en) * | 2000-12-27 | 2003-03-06 | Robarge Michael J. | Isoindole-imide compounds, compositions, and uses thereof |
| NZ548049A (en) * | 2003-12-02 | 2009-01-31 | Celgene Corp | Methods and compositions for the treatment and management of hemoglobinopathy and anemia |
| CN1968695A (zh) * | 2004-04-14 | 2007-05-23 | 细胞基因公司 | 含有用于治疗和控制骨髓发育不良综合征的免疫调节化合物的组合物和使用方法 |
| ES2434946T3 (es) * | 2005-08-31 | 2013-12-18 | Celgene Corporation | Compuestos de isoindol imida y composiciones que los comprenden y métodos para usarlo |
| WO2008073687A2 (en) * | 2006-12-08 | 2008-06-19 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| EP2358697B1 (en) | 2008-10-29 | 2015-10-21 | Celgene Corporation | Isoindoline compounds for use in the treatment of cancer. |
| CN101580501B (zh) * | 2009-06-01 | 2011-03-09 | 南京卡文迪许生物工程技术有限公司 | 3-(取代二氢异吲哚酮-2-基)-2,6-哌啶二酮的合成方法及其中间体 |
| CN119591582A (zh) * | 2014-04-14 | 2025-03-11 | 阿尔维纳斯运营股份有限公司 | 基于酰亚胺的蛋白水解调节剂和相关使用方法 |
| EP3160486B1 (en) * | 2014-06-27 | 2020-11-18 | Celgene Corporation | Compositions and methods for inducing conformational changes in cereblon other e3 ubiquitin ligases |
| US9499514B2 (en) * | 2014-07-11 | 2016-11-22 | Celgene Corporation | Antiproliferative compounds and methods of use thereof |
| EP3455219A4 (en) | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| EP3679026A1 (en) | 2017-09-04 | 2020-07-15 | C4 Therapeutics, Inc. | Glutarimide |
| US11512080B2 (en) | 2018-01-12 | 2022-11-29 | Kymera Therapeutics, Inc. | CRBN ligands and uses thereof |
| CA3101338A1 (en) | 2018-06-13 | 2019-12-19 | Biotheryx, Inc. | Aminoamide compounds |
| WO2020006264A1 (en) * | 2018-06-29 | 2020-01-02 | Dana-Farber Cancer Institute, Inc. | Ligands to cereblon (crbn) |
-
2019
- 2019-06-27 WO PCT/US2019/039555 patent/WO2020006264A1/en not_active Ceased
- 2019-06-27 EP EP19827425.0A patent/EP3813829A4/en active Pending
- 2019-06-27 JP JP2020571833A patent/JP7321194B2/ja active Active
- 2019-06-27 CA CA3102214A patent/CA3102214A1/en active Pending
- 2019-06-27 KR KR1020217001892A patent/KR20210025061A/ko active Pending
- 2019-06-27 CN CN201980057157.9A patent/CN112638380B/zh active Active
- 2019-06-27 AU AU2019294835A patent/AU2019294835B2/en active Active
- 2019-06-27 US US17/255,734 patent/US11530219B2/en active Active
- 2019-06-27 KR KR1020257001993A patent/KR20250020690A/ko active Pending
-
2022
- 2022-11-11 US US17/985,415 patent/US12110292B2/en active Active
-
2023
- 2023-07-25 JP JP2023120536A patent/JP7631434B2/ja active Active
Also Published As
| Publication number | Publication date |
|---|---|
| JP7321194B2 (ja) | 2023-08-04 |
| US11530219B2 (en) | 2022-12-20 |
| JP7631434B2 (ja) | 2025-02-18 |
| JP2023139195A (ja) | 2023-10-03 |
| AU2019294835A1 (en) | 2020-12-17 |
| US20230312575A1 (en) | 2023-10-05 |
| EP3813829A4 (en) | 2021-12-08 |
| CN112638380A (zh) | 2021-04-09 |
| JP2021530451A (ja) | 2021-11-11 |
| KR20210025061A (ko) | 2021-03-08 |
| CN112638380B (zh) | 2024-05-24 |
| WO2020006264A1 (en) | 2020-01-02 |
| EP3813829A1 (en) | 2021-05-05 |
| US20210292325A1 (en) | 2021-09-23 |
| US12110292B2 (en) | 2024-10-08 |
| KR20250020690A (ko) | 2025-02-11 |
| AU2019294835B2 (en) | 2025-04-17 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| W00 | Other event occurred |
Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT Effective date: 20251217 |
|
| W00 | Other event occurred |
Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT Effective date: 20260129 |
|
| U13 | Renewal or maintenance fee not paid |
Free format text: ST27 STATUS EVENT CODE: N-1-6-U10-U13-U300 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: DEEMED ABANDONED - FAILURE TO RESPOND TO MAINTENANCE FEE NOTICE Effective date: 20260217 |